MODIFIED SACCHARIDES
    8.
    发明授权
    MODIFIED SACCHARIDES 有权
    改良剂SACCHARIDE

    公开(公告)号:EP2118145B1

    公开(公告)日:2017-05-17

    申请号:EP08737594.5

    申请日:2008-01-11

    摘要: Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): -O-X-Y (Ia) or -O-R 1 (Ib) wherein X is C(O), S(O) or SO 2 ; Y is NR 1 R 2 or R 3 ; R 1 is C 1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R 2 is H or C 1-6 alkyl; and R 3 is C 1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.

    摘要翻译: 在相应的天然荚膜糖的至少一个单糖单元上的羟基位置上含有封闭基团的改性荚膜糖,其中所述封闭基团为式(Ia)或(Ib):-OXY(Ia)或 - OR 1(Ib)其中X为C(O),S(O)或SO 2; Y是NR 1 R 2或R 3; R 1是独立地选自羟基,巯基和胺的1,2或3个基团取代的C 1-6烷基; R 2是H或C 1-6烷基; 和R 3是C 1-6烷基; 用阻聚基修饰荚膜糖的方法; 包含修饰的荚膜糖的糖 - 蛋白质缀合物; 制备糖 - 蛋白质缀合物的方法,包含改性荚膜糖和/或糖 - 蛋白质缀合物的药物组合物; 以及相同的方法和用途。